The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor that regulates gene expression in a range of cells, including immune and epithelial cells. AhR signaling plays important roles in the immune system in both health and disease states. Tapinarof is a first-in-class small-molecule topical therapeutic AhR modulating agent launched for the treatment of psoriasis. To improve the activity and chemical stability of Tapinarof, a series of 2-phenylchromen-4-one derivatives were designed, synthesized and evaluated as novel AhR agonists. Compounds 5a, 5c, 5e and 5f potently activated AhR with an EC₅₀ value of 7, 9, 6 and 6 nmol·L^-1, respectively, which are 10-14 fold more potent than Tapinarof. Compounds 5a and 5e exhibit comparable inhibitory effects on IFN-γ production as Tapinarof. Furthermore, compounds 5a-5f exhibited favorable photochemical stability compared to Tapinarof. The compounds may eventually serve as lead compounds for the development of new AhR agonists.

Objective: To investigate the influencing factors for myopia among primary and secondary school students in Suzhou, so as to provide basis for myopia prevention and control. Methods: The students in Grade 4-12 were recruited by stratified cluster random sampling method. Gender, grade, parents＇ myopia history, outdoor activity time and video display terminal time were collected through the questionnaire of National Surveillance Program of Influencing Factors for Common Diseases and Health in Students. Uncorrected visual acuity and cycloplegic refraction were tested. Multivariate logistic regression analysis was performed to explore myopia-related factors. Results: A total of 990 questionnaires were distributed, and 882 valid questionnaires were recovered, with an effective rate of 89.09%. The prevalence rate of myopia was 78.23% ( 690 cases ). Multivariate logistic regression analysis showed that females ( OR=1.703, 95%CI: 1.173-2.474 ) , middle school students ( OR:5.597-11.949, 95%CI: 3.573-28.349 ) , both parents＇myopia ( OR=2.445, 95%CI: 1.597-3.742 ) , video display terminal time over 3 hours per day ( OR=2.026, 95%CI: 1.235-3.325 ) were risk factors for myopia; outdoor activity time over 2 hours per day ( OR: 0.493-0.510, 95%CI: 0.273-0.943 ) was a protective factor for myopia. Conclusion The prevalence of myopia among primary and secondary school students in Suzhou is 78.23%. Gender, grade, parents＇ myopia history, outdoor activity time and video display terminal time are influencing factors for myopia.

Animals ; Cytochrome P-450 CYP1A2 ; Cytochrome P-450 CYP2C19 ; metabolism ; Cytochrome P-450 Enzyme System ; metabolism ; Cytochromes ; metabolism ; Liver Cirrhosis ; enzymology ; Rats

The paper is aimed to establish a methods for identication of pearl powder and conch powder from different origins. Hermetic aluminum pan was used to encapsulate samples. The optimal testing conditions were: heating rate 10 degrees C x min(-1), sample weight 3 mg and nitrogen gas flow rate 40 mL x min(-1). The enthalpy values of pearl powder and conch powder was obvious different. Identication of pearl powder and conch powder by DSC is a practical method for its accuracy, convenience and practificality.
Animal Shells ; chemistry ; Animals ; Calorimetry, Differential Scanning ; methods ; China ; Discriminant Analysis ; Pinctada ; chemistry ; classification ; Powders ; chemistry

OBJECTIVETo investigate the influence of the time interval from the end of semen processing to artificial intrauterine in semination with husband's sperm (AIH-IUI) on the rate of clinical pregnancy.

METHODSThis study involved 191 AIH-IUI cycles with the same ovulation induction protocol. After Percoll density gradient centrifugation, we divided the sperm into four groups based on the incubation time: 0-19, 20-39, 40-59, and 60-80 min, and again into another four groups according to the total progressively motile sperm count (TPMC): (0-9), (10-20), (21-30), and > 30 x 10(6). We analyzed the correlation of the clinical pregnancy rate with the time interval from the end of sperm processing to AIH-IUI and with other influencing factors, such as maternal age, infertility duration, and semen quality.

RESULTSThe rate of clinical pregnancy was significantly higher in the 20-39 min group (18.3%) than in the 0-19, 40-59, and 60-80 min groups (12.7, 11.4 and 9.1%) (all P < 0.05). The (10-20) x 10(6) group achieved a remarkably higher pregnancy rate (16.7%) than the (0-9), (21-30), and > 30 x 10(6) groups (0, 11.4, and 8.3%) (all P < 0.05). Logistic multivariate analysis showed that the rate of clinical pregnancy was decreased with the increased age of the women (OR 0.89, 95% CI 0.83-0.94) but significantly elevated in the 20-39 min group (OR 2.11, 95% CI 1.34-3.13) and of (10-20) x 10(6) group (OR 2.06, 95% CI 1.32-3.46).

CONCLUSIONThe time interval from the end of sperm processing to AIH-IUI is a most significant factor influencing the rate of clinical pregnancy of AIH-IUI.

Centrifugation, Density Gradient ; Female ; Humans ; Infertility ; therapy ; Insemination, Artificial, Homologous ; statistics & numerical data ; Male ; Pregnancy ; Pregnancy Rate ; Semen ; Semen Analysis ; Sperm Count ; Spermatozoa ; Time Factors

BACKGROUND:Antibiotic loaded bone cement has been well studied in clinical prevention and treatment of postoperative infection after artificial joint replacement. However, little is reported on antituberculotic-loaded bone cement. OBJECTIVE:To investigate the drug release properties of polymethyl methacrylate bone cement carrying antituberculosis drugs in a simulated body fluid (phosphate buffer solution, PBS). METHODS:The bone cement SimpLex P and antituberculosis drugs, including pyrazinamide, isoniazid, rifapentine, prothionamide, capreomycin, rifampicin, moxifloxacin, and amikacin, were mixed at 40 g:1.5 g and 40 g: 2.5 g ratios to prepare 16 groups of experimental specimens (n=5 per group). In addition, 40 g of bone cement powder was mixed with the liquid monomer to prepare a group of non-loaded bone cement specimens (control group,n=5). Either experimental or control specimens were soaked in PBS simulated body fluid, and then the extractions were taken at different time points to measure concentrations of antituberculosis drugs by high performance liquid chromatography. RESULTS AND CONCLUSION:The effective sustained-releasing time in the PBS simulated body fluid was 45 and 60 days for 1.5 g and 2.5 g groups of pyrazinamide, was 60 and 45 days for 1.5 g and 2.5 g groups of isoniazid, was 60 and 45 days for 1.5 g and 2.5 g groups of rifapentine, was 150 and 150 days for 1.5 g and 2.5 g groups of protionamide, was 150 and 150 days for 1.5 g and 2.5 g groups of capreomycin, was 45 and 60 days for 1.5 g and 2.5g groups of rifampicin, was 90 and 90 days for 1.5 g and 2.5 g groups of moxifloxacin, and was 60 and 90 days for 1.5 g and 2.5 g groups of amikacin, respectively. All the drug carriers had good drug release characteristics. Especially the 1.5 g and 2.5 g groups of protionamide, 1.5 g and 2.5 g groups of capreomycin, 1.5 g and 2.5 g groups of moxifloxacin and 2.5 g group of amikacin showed a longer period of drug release in accordance with the clinical need. However, our preliminary findings showed that the mechanical strength of the composite bone cement was considerably reduced by isoniazid, rifampicin, rifapentine, or protionamide, while the SimpLex P bone cement carrying pyrazinamide, amikacin, moxifloxacin, or capreomycin showed no changes in the mechanical strength. Therefore, pyrazinamide, amikacin, moxifloxacin, and capreomycin are suitable for the preparation of bone cements carrying antituberculosis drugs.

The catalytic generation of H2 in living cells provides a method for antioxidant therapy.In this study,an[FeFe]-hydrogenase mimic[Ru+Fe2S2@F127(80)]was synthesized by self-assembling polymeric plur-onic F-127,catalytic[Fe2S2]sites,and photosensitizer Ru(bpy)32+.Under blue light irradiation,hydrated protons were photochemically reduced to H2,which increased the local pH in living cells(HeLa cells).The generated H2 was subsequently used as an antioxidant to decrease reactive oxygen species(ROS)levels in living cells(HEK 293T,HepG2,MCF-7,and HeLa cells).Our findings revealed that the proliferation of HEK 293T cells increased by a factor of about six times,relative to that of other cells(HepG2,MCF-7,and HeLa cells).Intracellular ROS and pH levels were then monitored using fluorescent cell imaging.Our study showed that cell imaging can be used to evaluate the ability of Ru+Fe2S2@F127 to eliminate oxidative stress and prevent ROS-related diseases.

OBJECTIVETo investigate the intervention effect of Danggui Shaoyao San on rats with cirrhotic ascites, and discuss the effect of arginine vasopressin (AVP) on cirrhotic ascites.

METHODMale SD rats were randomly divided into the control group, the model group, Danggui Shaoyao San low, middle and high dose groups. The cirrhotic ascites rat model was established by CCl4 combined with phenobarbital. Their urines were collected at 24 h to observe urine excretion of each group. Filter papers were used to determine the amount of ascites. The levels of serum alanine aminotransferasa (ALT) , aspartate aminotransferase (AST) were detected by the automatic biochemistry analyzer. Plasma prothrombin time (PT) was evaluated by the blood coagulation analyzer. The concentration of AVP in plasma was detected by enzyme-linked immunosorbent assay (ELISA). Pathological changes in livers were observed by HE staining.

RESULTCompared with the model group, the Danggui Shaoyao San group showed significant improvement in live indexes, with notable decrease in serum ALT and AST and the time of PT, improvement in liver pathological changes. Simultaneously, the amount of ascites decreased to varying degrees, with notable increase in urine in 24 h and decrease in AVP concentration in plasma.

CONCLUSIONDanggui Shaoyao San can notably improve liver functions of rats with cirrhotic ascites, reduce the generation of ascites and delay the progress of liver pathological changes. Its mechanism may be related to AVP.

Animals ; Arginine Vasopressin ; blood ; Ascites ; blood ; complications ; drug therapy ; physiopathology ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Liver ; drug effects ; enzymology ; metabolism ; physiopathology ; Liver Cirrhosis ; complications ; Male ; Rats ; Rats, Sprague-Dawley

Adolescent ; Adult ; Antiviral Agents ; therapeutic use ; DNA, Viral ; blood ; Female ; Hepatitis B virus ; genetics ; Hepatitis B, Chronic ; drug therapy ; virology ; Humans ; Male ; Middle Aged ; Nucleosides ; therapeutic use ; Pyrimidinones ; therapeutic use ; Thymidine ; analogs & derivatives ; Young Adult

OBJECTIVETo assess the association between polymorphisms within the interferon-Gamma receptor gene(IFN-GammaR) and systemic lupus erythematosus (SLE) in Chinese people.

METHODSThe IFN-GammaR genotypes of 94 SLE patients and 80 healthy subjects were examined by the reverse transcription-polymerase chain reaction (RT-PCR)-single-strand conformation polymorphism (SSCP) method, RT-PCR-restriction fragment length polymorphism (RFLP) method and DNA sequencing.

RESULTSThere was no statistically significant difference in the IFN-GammaR genotype frequencies between the two groups. The IFN-Gamma R2 Arg64/Arg64 genotype decreased the risk of SLE (OR = 2.481, 95% CI 0.992 - 6.203, P = 0.047). The decreased risk of the development of SLE was detected in the individuals who had the combination of IFN-GammaR2 Arg64/Arg64 genotype and IFN-GammaR1 Val14/Val14 genotype (OR = 2.481, 95% CI 0.992 - 6.203, P = 0.047).

CONCLUSIONThe IFN-GammaR2 Arg64/Arg64 genotype does not determine susceptibility to SLE in Chinese people, and the combination of IFN-Gamma R2 Arg64/Arg64 genotype and IFN-Gamma R1 Val14/Val14 genotype does not, either.

Adolescent ; Adult ; Base Sequence ; Female ; Genetic Predisposition to Disease ; genetics ; Genotype ; Humans ; Lupus Erythematosus, Systemic ; genetics ; Male ; Middle Aged ; Polymorphism, Genetic ; genetics ; Polymorphism, Single-Stranded Conformational ; Receptors, Interferon ; genetics ; Reverse Transcriptase Polymerase Chain Reaction ; Sequence Analysis, DNA